Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice

YANG Min1; 2 WANG Guangji1 XIANG Jingde2 XU Yuping2 WANG Songpei2  LI Xiaomin2 PAN Shangren2 XU Xijie2 YE Wencai3  1

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Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice

更新时间：2021-03-12

- Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice
- NUCLEAR TECHNIQUES Issue 12, (2005)
- 作者机构：
  
  1. 中国药科大学药代中心
  2. 江苏省原子医学研究所无锡,214063
  3. 中国药科大学天然药化教研室,南京,210009
- 作者简介：
- 基金信息：
  
  国家高技术研究发展计划(863计划)(2003AA2Z347A)资助;江苏省自然基金资助(BK2004025)
- DOI：
  CLC： R96;R943
- Published：01 December 2005
- 稿件说明：
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[1]杨敏,王广基,项景德,徐宇平,王颂佩,李晓敏,潘尚仁,徐希杰,叶文才.氚标记23-羟基白桦酸的制备及其在动物体内的评价[J].核技术,2005(12):929-933.

YANG Min1, 2 WANG Guangji1 XIANG Jingde2 XU Yuping2 WANG Songpei2 LI Xiaomin2 PAN Shangren2 XU Xijie2 YE Wencai3 1. Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice[J]. Nuclear techniques, 2005, (12): 929-933.
[1]杨敏,王广基,项景德,徐宇平,王颂佩,李晓敏,潘尚仁,徐希杰,叶文才.氚标记23-羟基白桦酸的制备及其在动物体内的评价[J].核技术,2005(12):929-933. DOI：

YANG Min1, 2 WANG Guangji1 XIANG Jingde2 XU Yuping2 WANG Songpei2 LI Xiaomin2 PAN Shangren2 XU Xijie2 YE Wencai3 1. Preparation of 3H-23-hydroxylbetulinic acid and in vivo evaluations in mice[J]. Nuclear techniques, 2005, (12): 929-933. DOI：

摘要

制备氚标23-羟基白桦酸（3H-23-HBA）

并对其在正常鼠及荷瘤鼠的体内分布进行初步探索。23-HBA经23位氧化、硼氚化钠还原后制得3H-23-HBA

考察了标记物的纯度和稳定性

并在ICR小鼠、接种肝癌HepA肿瘤的小鼠体内研究其生物分布特征。结果显示:（1）所得标记物放射化学纯度>95%

放射性比活度为3.33×105Bq/μg（23-HBA）;（2）标记化合物的四氢呋喃溶液在–20℃稳定;（3）小鼠尾静脉注射3H-23-HBA（10mg/kg

3.7×105Bq/只）后

在血中清除慢

血浆中原形药约占60%;（4）小鼠尾静脉注射3H-23-HBA（10mg/kg

3.7×105Bq/只）后

在胆、肝、肠浓聚

消除慢;肿瘤鼠肺、胆中摄取高于正常鼠

尤其是胆

至注射后8h仍高达106.89%±47.4%ID/g。实体瘤与对侧肌肉组织的摄取比约为2。3H-23-HBA纯度高

稳定性好

适用于23-HBA药代动力学研究。

Abstract

The purpose of this work is to study the preparation and pharmacokinetics in mice of tritium-labeled 23-hydroxylbetulinic acid (3H-23-HBA). 3H-23-HBA was synthesized by oxidation with manganese and deoxidization with tritium-labelled sodium borohydride. The purity and stability of 3H-23-HBA were evaluated by HPLC and TLC

and the dynamic distribution in ICR mice and liver cancer HepA tumor-bearing mice were studied. The results showed that the radiochemical purity was over 95% and the specific radioactivity was 3.33×105 Bq/μg (23-HBA); 3H-23-HBA in tetrahydrofuran was stable at –20℃; 3H-23-HBA cleared slowly in blood (MRT=32.68 h) and about 60% of the total radioactivity in plasma was contributed by 23-HBA; and 3H-23-HBA was concentrated in gallbladder

liver and small intestine. In tumor-bearing mice

the uptakes of lung and gallbladder were higher than the normal mice

especially in the gallbladder. At 8 h post intravenous injection

the uptake of gallbladder was still as high as 106.89%±47.4%ID/g organ. The tumor-to-muscle ratio was about 2. The purity of 3H-23-HBA is high and 3H-23-HBA is stable. So 3H-23-HBA appears to be fit for the pharmacokinetic study of 23-HBA.

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